A radioimmunoassay for the anticonvulsant and neuroprotective agent, MK-801.
A radioimmunoassay is described for MK-801, a potent anticonvulsant and neuroprotective agent. Two immunogens were prepared from N-glutaryl- and N-carboxyethyl-MK-801 by coupling through their carboxyl groups to bovine serum albumin. Radioligands were I-125-iodotyramine conjugates of the same derivatives. Both types of antisera displayed bridge recognition which could be circumvented. In the first case, specificity for N-acyl derivatives was satisfied by acetylating the analyte prior to measurement. Antisera to the N-alkyl derivative yielded a satisfactory assay for MK-801 when the heterologous radioligand was employed. The first of these strategies was adopted for the routine assay. Specificity relative to hydroxylated metabolites was a function both of antiserum selectivity and sample preparation. High plasma concentrations of drugs concomitantly administered to epileptics posed special analytical problems. Assay sensitivity is 40 pg/ml in plasma and the interassay CV is about 5%.
Hichens
M
M
Department of Drug Metabolism, Merck Sharp & Dohme Research Laboratories, West Point, PA 19486.
Greber
T F
TF
Vyas
K P
KP
D003429:Cross Reactions; D016291:Dizocilpine Maleate / Q000008:administration & dosage / Q000032:analysis* / Q000097:blood; D004827:Epilepsy / Q000097:blood / Q000188:drug therapy; D005069:Evaluation Studies as Topic; D006801:Humans; D011863:Radioimmunoassay / Q000379:methods*; D012680:Sensitivity and Specificity
D016291:Dizocilpine Maleate